Synthesis and α-glucosidase inhibition activity of dihydroxy pyrrolidines.
Bioorg Med Chem Lett
; 27(12): 2818-2823, 2017 06 15.
Article
en En
| MEDLINE
| ID: mdl-28495082
ABSTRACT
A new series of Deacetylsarmentamide A and B derivatives, amides and sulfonamides of 3,4-dihydroxypyrrolidines as α-glucosidase inhibitors were designed and synthesized. The biological screening test against α-glucosidase showed that some of these compounds have the positive inhibitory activity against α-glucosidase. Saturated aliphatic amides were more potent than the olefinic amides. Among all the compounds, 5o/6o having polar -NH2 group, 10f/11f having polar -OH group on phenyl ring displayed 3-4-fold more potent than the standard drugs. Acarbose, Voglibose and Miglitol were used as standard references. The promising compounds 6i, 5o, 6o, 10a, 11a, 10f and 11f have been identified. Molecular docking simulations were done for compounds to identify important binding modes responsible for inhibition activity of α-glucosidase.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Pirrolidinas
/
Inhibidores de Glicósido Hidrolasas
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2017
Tipo del documento:
Article
País de afiliación:
India